Assay Detail
Binding
CHEMBL856827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]MK-499 from hERG potassium channel expressed in HEK293 cells
33
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 32 | - | - |
| IC50 | 1 | 6.89 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48029 | — | — | 2 | 6.89 |
| CHEMBL218068 | — | — | 1 | - |
| CHEMBL218478 | — | — | 1 | - |
| CHEMBL374658 | — | — | 1 | - |
| CHEMBL438994 | — | — | 1 | - |
| CHEMBL218075 | — | — | 1 | - |
| CHEMBL218460 | — | — | 1 | - |
| CHEMBL217955 | — | — | 1 | - |
| CHEMBL217992 | — | — | 1 | - |
| CHEMBL217904 | — | — | 1 | - |
| CHEMBL217940 | — | — | 1 | - |
| CHEMBL386184 | — | — | 1 | - |
| CHEMBL218211 | — | — | 1 | - |
| CHEMBL218713 | — | — | 1 | - |
| CHEMBL218104 | — | — | 1 | - |
| CHEMBL425642 | — | — | 1 | - |
| CHEMBL218546 | — | — | 1 | - |
| CHEMBL219060 | — | — | 1 | - |
| CHEMBL218017 | — | — | 1 | - |
| CHEMBL218067 | — | — | 1 | - |
| CHEMBL220660 | — | — | 1 | - |
| CHEMBL425462 | — | — | 1 | - |
| CHEMBL218547 | — | — | 1 | - |
| CHEMBL219113 | — | — | 1 | - |
| CHEMBL219114 | — | — | 1 | - |
| CHEMBL221133 | — | — | 1 | - |
| CHEMBL221605 | — | — | 1 | - |
| CHEMBL374865 | — | — | 1 | - |
| CHEMBL218275 | — | — | 1 | - |
| CHEMBL435316 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48029 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL217955 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218104 | — | Activity | = | 9200.0 | nM | - |
| CHEMBL218713 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218211 | — | Activity | = | 5200.0 | nM | - |
| CHEMBL386184 | — | Activity | = | 5800.0 | nM | - |
| CHEMBL217940 | — | Activity | = | 4200.0 | nM | - |
| CHEMBL217904 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL217992 | — | Activity | = | 5000.0 | nM | - |
| CHEMBL425642 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218460 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218075 | — | Activity | = | 470.0 | nM | - |
| CHEMBL438994 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL374658 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218478 | — | Activity | = | 3100.0 | nM | - |
| CHEMBL218463 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL217915 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL48029 | — | Activity | = | 110.0 | nM | - |
| CHEMBL218068 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218546 | — | Activity | = | 9600.0 | nM | - |
| CHEMBL219060 | — | Activity | = | 960.0 | nM | - |
| CHEMBL218017 | — | Activity | = | 2900.0 | nM | - |
| CHEMBL218067 | — | Activity | = | 2300.0 | nM | - |
| CHEMBL220660 | — | Activity | = | 4200.0 | nM | - |
| CHEMBL435316 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218547 | — | Activity | = | 1070.0 | nM | - |
| CHEMBL219113 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL219114 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL221133 | — | Activity | = | 6100.0 | nM | - |
| CHEMBL221605 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL374865 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL425462 | — | Activity | > | 10000.0 | nM | - |
| CHEMBL218275 | — | Activity | > | 10000.0 | nM | - |